Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery |
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| Authors: | Hu Qi-da Fan Hui Lou Wei-jian Wang Qing-qing Tang Gu-ping |
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| Institution: | Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou, China. |
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| Abstract: | Polyethylenimine-cyclodextrin-tegafur (PEI-CyD-tegafur) conjugate was synthesized as a novel multifunctional prodrug of tegafur
for co-delivery of chemotherapeutic agent tegafur and enhanced green fluorescent protein (EGFP) reporter plasmid DNA. Conjugation
of tegafur to PEI-CyD via chemical linkage was characterized by 1H NMR spectrometry and ultraviolet (UV) spectrometry. PEI-CyD-tegafur was able to condense plasmid DNA into complexes of around
150 nm with positive charge at the N/P ratio of 25, in accordance with electron microscopy observation of compact and monodisperse
nanoparticles. The results of in vitro experiments showed enhanced cytotoxicity and considerable transfection efficiency in
B16F10 cell line. Therefore, PEI-CyD-tegafur may have great potential as a co-delivery system with anti-cancer activity and
potential for gene delivery. |
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| Keywords: | Polyethylenimine β-Cyclodextrin Tegafur Co-delivery Gene therapy |
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